Resp Drugs Flashcards
What is the mechanism of a beta-2-adrenoceptor agonist?
beta 2 receptors are coupled with Gs proteins
Agonist binding stimulates adenylyl cyclase which converts ATP into cAMP
Phosphodiesterase breaks down cAMP
Decrease intracellular Ca levels and increase formation of protein kinase A
Protein kinase A phosphorylates myosin light chain kinase which brings about relaxation of bronchi smooth muscle
What is an example of a SABA?
Salbutamol
Example of a LABA?
Salmeterol
Formoterol
What are side effects of beta-2-agonists?
Fine tremor
Hypotension
Tachycardia
Where are CysLTs derived from?
Mast cells
Explain the mechanism behind leukotriene release form mast cells.
Mast cells produce arachidonic acid by stimulation of phospholipase A2
Stimulation of 5-lopooxygenase by FLAP enzyme
Release of leukotirienes which bind to CysLT1
CysLT1 Antagonists prevent?
Muscle contraction, mucous secretion and oedema
What are examples of CysLT1 receptor antagonists?
Montelukast
Zafirlukast
What are side effects of CysLT1 Receptor Antagonists?
Abdominal Pain
Headaches
What are examples of xanthines?
Theophylline
Aminophylline
What is the mechanism of xanthines?
Inhibit phosphodiesterase which increases cAMP levels (breakdown of cAMP in inhibited)
Decreases protein kinase A
What are side effects of xanthines?
Nausea
Vomiting
Abdominal discomfort
Headache
What is the mechanism of a corticosteroid?
Signalling via nuclear receptors GR-alpha where glucocorticoid binds and enters the nucleus
Binds to promotor region and either produces transactivation or trans repression of genes the control inflammation
Which genes are induced by corticosteroids?
Annexin 1 - inhibits synthesis of phospholipase A1
Decrease formation of arachidonic acid and decreases production of leukotrienes, chemotaxis and spasmogens
Which genes are repressed by corticosteroids?
Cytokines
Decrease formation of IL 4, 5, 7, and 13
Eosinophils and plasma cells (IgE) are not recruited